Assay Detail
Functional
CHEMBL4146241
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Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.92 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 8.54 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.97 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.24 |
| CHEMBL4168868 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286830 | LORLATINIB | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 57.5 | nM | 7.24 |
| CHEMBL4168868 | — | IC50 | < | 1.5 | nM | - |